AM6545 | CB1R antagonist | Probechem Biochemicals

Chemical Structure : AM6545

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AM6545 (AM 6545)

货号: PC-20077Not For Human Use, Lab Use Only.

AM6545 (AM-6545) is a potent, selective, oral bioavailable and non-brain-penetrant neutral CB1R antagonist with Ki of 3.3 nM, >100-fold selectivity over CB2R.

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生物&药学活性

AM6545 (AM-6545) is a potent, selective, oral bioavailable and non-brain-penetrant neutral CB1R antagonist with Ki of 3.3 nM, >100-fold selectivity over CB2R.
Unlike rimonabant, AM6545 does not reduce GTPγS binding in mouse brain membranes and is therefore a neutral antagonist.
AM6545 (10 mg/kg/d for 28 days, oral) improved the metabolic profile in mice with diet-induced obesity (DIO).
AM6545 exhibited therapeutically relevant efficacy in reducing weight and improving hormonal/metabolic abnormalities in animal models of obesity.
AM6545 (4.0, 8.0 and 16.0 mg/kg, i.p.) significantly reduced food-reinforced operant responding in vivo.

物理化学性质&存储条件

分子量	556.46
分子式	C26H23Cl2N5O3S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	5-(4-[4-cyanobut-1-ynyl]phenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(1,1-dioxo-thiomorpholino)-1H-pyrazole-3-carboxamide

参考文献

1. Tam J, et al. J Clin Invest. 2010 Aug;120(8):2953-66.

2. Randall PA, et al. Pharmacol Biochem Behav. 2010 Nov;97(1):179-84.

3. Limebeer CL, et al. Br J Pharmacol. 2010 Sep;161(2):336-49.

AM6545 (AM 6545)

生物&药学活性

物理化学性质&存储条件

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AM6545 (AM 6545)

生物&药学活性

物理化学性质&存储条件

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